公开(公告)号：JP2000159792A

公开(公告)日：2000-06-13

申请号：JP33077099

申请日：1999-11-22

Applicant: HOFFMANN LA ROCHE

Inventor： BURDICK DAVID CARL ,  MOINE GERARD ,  RAEDERSTORFF DANIEL ,  WEBER PETER

IPC: A23D9/013 ,  A23L1/30 ,  A23L33/20 ,  A61K31/56 ,  A61K31/575 ,  A61P3/04 ,  A61P3/06 ,  C07J9/00 ,  C11B1/00 ,  A23L1/307

Abstract: PROBLEM TO BE SOLVED: To obtain the subject compound capable of remarkably reducing both serum cholesterol and triglyceride by producing the compound from a phytosterol and/or a phytostanol and a specific polyunsaturated fatty acid. SOLUTION: This phytosterol and/or phytostanol derivative comprises (A) a phytosterol and/or a phytostanol and (B) a 18-22C polyunsaturated fatty acid containing at least 3 unsaturated carbon-carbon double bonds. β-Sitosterol is preferable as the component A. Eicosapentaenoic acid or docosahexaenoic acid is preferable as the component B. The objective compound is obtained, for example, by transesterifying the liberated component A with the polyunsaturated fatty acid ester. The reaction is preferably carried out by using a sodium alkoxide of a 1-4C alcohol as a catalyst in the absence of a reaction solvent at 80-140 deg.C under 133-6650 Pa.

公开(公告)号：AU2018337597A1

公开(公告)日：2020-03-26

申请号：AU2018337597

申请日：2018-09-19

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM JEAN-MICHEL ,  FANTASIA SERENA MARIA ,  FISHLOCK DANIEL VINCENT ,  HOFFMANN-EMERY FABIENNE ,  MOINE GERARD ,  PFLEGER CHRISTOPHE ,  MOESSNER CHRISTIAN

IPC: C07D471/04 ,  C07D519/00

Abstract: The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[l,2- b]pyridazin-6-yl)pyrido[l,2-a]pyrimidin-4-one derivatives useful pharmaceutically active compounds.

公开(公告)号：DE602006002612D1

公开(公告)日：2008-10-16

申请号：DE602006002612

申请日：2006-05-15

Applicant: HOFFMANN LA ROCHE

Inventor： ABRECHT STEFAN ,  ADAM JEAN-MICHEL ,  FETTES ALEC ,  FORICHER JOSEPH ,  LOHRI BRUNO ,  MATTEI PATRIZIO ,  MOINE GERARD ,  SCHMID RUDOLF ,  ZUTTER ULRICH

IPC: C07D307/32 ,  C07D307/38

Abstract: This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula and with its use for the manufacture of pyrido[2,1-a]isoquinoline derivatives of the formula which are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

公开(公告)号：NO995784L

公开(公告)日：2000-05-29

申请号：NO995784

申请日：1999-11-25

Applicant: HOFFMANN LA ROCHE

Inventor： BURDICK DAVID CARL ,  MOINE GERARD ,  RAEDERSTORFF DANIEL ,  WEBER PETER

IPC: A23D9/013 ,  A23L1/30 ,  A23L33/20 ,  A61K31/56 ,  A61K31/575 ,  A61P3/04 ,  A61P3/06 ,  C07J9/00 ,  C11B1/00 ,  A23D9/00

Abstract: Phytosterol and/or phytostanol esters with polyunsaturated fatty acids having from 18 to 22 carbon atoms and at least three carbon-carbon double bonds are effective in reducing both serum cholesterol and trglycerides.

公开(公告)号：NO995784A

公开(公告)日：2000-05-29

申请号：NO995784

申请日：1999-11-25

Applicant: HOFFMANN LA ROCHE

Inventor： BURDICK DAVID CARL ,  MOINE GERARD ,  RAEDERSTORFF DANIEL ,  WEBER PETER

IPC: A23L1/307 ,  A23D9/013 ,  A23L1/30 ,  A61K31/56 ,  A61K31/575 ,  A61P3/04 ,  A61P3/06 ,  C07J9/00 ,  C11B1/00 ,  A23D9/00

CPC classification number: A61K31/56 ,  A23D9/013 ,  A23L33/11

公开(公告)号：CA2290331A1

公开(公告)日：2000-05-26

申请号：CA2290331

申请日：1999-11-19

Applicant: HOFFMANN LA ROCHE

Inventor： WEBER PETER ,  MOINE GERARD ,  RAEDERSTORFF DANIEL ,  BURDICK DAVID CARL

IPC: A23D9/013 ,  A23L1/30 ,  A23L33/20 ,  A61K31/56 ,  A61K31/575 ,  A61P3/04 ,  A61P3/06 ,  C07J9/00 ,  C11B1/00 ,  A61P3/02 ,  A23L1/307

Abstract: Phytosterol and/or phytostanol esters with polyunsaturated fatty acids having from 18 to 22 carbon atoms and at least three carbon-carbon double bonds are effective in reducing both serum cholesterol and trglycerides.

公开(公告)号：CA2607927A1

公开(公告)日：2006-11-30

申请号：CA2607927

申请日：2006-05-15

Applicant: HOFFMANN LA ROCHE

Inventor： MOINE GERARD ,  SCHMID RUDOLF ,  ZUTTER ULRICH ,  ADAM JEAN-MICHEL ,  LOHRI BRUNO ,  MATTEI PATRIZIO ,  ABRECHT STEFAN ,  FETTES ALEC ,  FORICHER JOSEPH

IPC: C07D307/32 ,  C07D307/38

Abstract: This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula and with its use for the manufacture of pyrido[2,1-a]isoquinoline derivatives of the formula which are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

公开(公告)号：AU762539B2

公开(公告)日：2003-06-26

申请号：AU6065599

申请日：1999-11-25

Applicant: HOFFMANN LA ROCHE

Inventor： BURDICK DAVID CARL ,  MOINE GERARD ,  RAEDERSTORFF DANIEL ,  WEBER PETER

IPC: A23D9/013 ,  A23L1/30 ,  A23L33/20 ,  A61K31/56 ,  A61K31/575 ,  A61P3/04 ,  A61P3/06 ,  C07J9/00 ,  C11B1/00 ,  C07J1/00 ,  A61K31/565

Abstract: Phytosterol and/or phytostanol esters with polyunsaturated fatty acids having from 18 to 22 carbon atoms and at least three carbon-carbon double bonds are effective in reducing both serum cholesterol and trglycerides.

公开(公告)号：SG11202002610TA

公开(公告)日：2020-04-29

申请号：SG11202002610T

申请日：2018-09-19

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM JEAN-MICHEL ,  FANTASIA SERENA MARIA ,  FISHLOCK DANIEL VINCENT ,  HOFFMANN-EMERY FABIENNE ,  MOINE GERARD ,  PFLEGER CHRISTOPHE ,  MOESSNER CHRISTIAN

IPC: C07D471/04 ,  C07D519/00

Abstract: The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.

公开(公告)号：AR112828A1

公开(公告)日：2019-12-18

申请号：ARP180102704

申请日：2018-09-21

Applicant: HOFFMANN LA ROCHE

Inventor： MOESSNER CHRISTIAN ,  PFLEGER CHRISTOPHE ,  MOINE GERARD ,  HOFFMANN-EMERY FABIENNE ,  FISHLOCK DANIEL VINCENT ,  FANTASIA SERENA MARIA ,  ADAM JEAN-MICHEL

IPC: C07D471/04 ,  C07D519/00

Abstract: La presente solicitud se refiere a un proceso para la preparación de derivados de 7-(4,7-diazaespiro[2,5]octan-7-il)-2-(2,8-dimetilimidazo[1,2-b]piridazin-6-il)pirido[1,2-a]pirimidin-4-ona útiles como compuestos farmacéuticamente activos. Reivindicación 1: Un proceso para la preparación de un compuesto de fórmula (1) o la sal de HCl del mismo, que comprende hacer reaccionar un compuesto de fórmula (2) con un ácido fuerte, en particular HCl. Reivindicación 15: Un compuesto de fórmula (2). Reivindicación 16: Un compuesto de fórmula (3), en la que X es un sulfonato de alquilo o arilo (tal como pTolSO₃-, CH₃SO₃-, fenil-SO₃), sulfonatos de alquilo o arilo fluorados (tal como CF₃SO₃-, nonaflato), o un haluro (tal como Cl, Br o I). Reivindicación 17: Un compuesto de fórmula (4).